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AR008386A1 - BENZIMIDAZOLE DERIVATIVES WITH ANTIHISTAMINE ACTIVITY AND ANTIHISTAMINE PHARMACEUTICAL COMPOSITION CONTAINING THEM. - Google Patents

BENZIMIDAZOLE DERIVATIVES WITH ANTIHISTAMINE ACTIVITY AND ANTIHISTAMINE PHARMACEUTICAL COMPOSITION CONTAINING THEM.

Info

Publication number
AR008386A1
AR008386A1 ARP970102441A ARP970102441A AR008386A1 AR 008386 A1 AR008386 A1 AR 008386A1 AR P970102441 A ARP970102441 A AR P970102441A AR P970102441 A ARP970102441 A AR P970102441A AR 008386 A1 AR008386 A1 AR 008386A1
Authority
AR
Argentina
Prior art keywords
antihistamine
pharmaceutical composition
composition containing
benzimidazole derivatives
activity
Prior art date
Application number
ARP970102441A
Other languages
Spanish (es)
Original Assignee
Faes Farma Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Faes Farma Sa filed Critical Faes Farma Sa
Publication of AR008386A1 publication Critical patent/AR008386A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pulmonology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen derivados del bencimidazol de formula (I) en donde R1 es H o un grupo carbonado de cadena corta tal como metilo, etilo, isopropilo,ciclopropilo o vinilo; R2 es un grupo seleccionado de entre los siguientes: CH2OH, COOH, COOR3 y4,4 -dimetil-2-oxazolinil, siendo R3 un grupo de cadenacorta tal como metilo, etilo, etc. tal como se ha definido para R1. Estos compuestos tienen una alta actividad antihistamínica H1 y antialérgica ycarecen de efectos centrales y sobre elsistema cardiovascular. Se describe también una composicion farmacéutica que contiene dichos compuestos.Derivatives of benzimidazole of formula (I) are described wherein R1 is H or a short-chain carbon group such as methyl, ethyl, isopropyl, cyclopropyl or vinyl; R2 is a group selected from the following: CH2OH, COOH, COOR3 and 4,4-dimethyl-2-oxazolinyl, R3 being a short chain group such as methyl, ethyl, etc. as defined for R1. These compounds have high antihistamine H1 and antiallergic activity and have no central and cardiovascular effects. A pharmaceutical composition containing such compounds is also described.

ARP970102441A 1996-06-04 1997-06-05 BENZIMIDAZOLE DERIVATIVES WITH ANTIHISTAMINE ACTIVITY AND ANTIHISTAMINE PHARMACEUTICAL COMPOSITION CONTAINING THEM. AR008386A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES09601236A ES2124167B1 (en) 1996-06-04 1996-06-04 NEW DERIVATIVES OF BENZMIDAZOLE WITH ANTIHISTAMINE ACTIVITY.

Publications (1)

Publication Number Publication Date
AR008386A1 true AR008386A1 (en) 2000-01-19

Family

ID=8295035

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP970102441A AR008386A1 (en) 1996-06-04 1997-06-05 BENZIMIDAZOLE DERIVATIVES WITH ANTIHISTAMINE ACTIVITY AND ANTIHISTAMINE PHARMACEUTICAL COMPOSITION CONTAINING THEM.

Country Status (27)

Country Link
US (1) US5877187A (en)
EP (1) EP0818454B1 (en)
JP (1) JP4218991B2 (en)
CN (1) CN1105716C (en)
AR (1) AR008386A1 (en)
AT (1) ATE264317T1 (en)
AU (1) AU725700B2 (en)
BR (1) BR9703276A (en)
CA (1) CA2206754C (en)
CZ (1) CZ289278B6 (en)
DE (2) DE69728608T2 (en)
DK (1) DK0818454T3 (en)
ES (1) ES2124167B1 (en)
FR (1) FR11C0023I2 (en)
HR (1) HRP970307B1 (en)
HU (1) HU227598B1 (en)
IN (1) IN186319B (en)
LU (1) LU91798I2 (en)
MX (1) MXPA97004127A (en)
NO (2) NO313195B1 (en)
PL (1) PL188908B1 (en)
PT (1) PT818454E (en)
RU (1) RU2182150C2 (en)
SI (1) SI0818454T1 (en)
TR (1) TR199700464A3 (en)
TW (1) TW438794B (en)
ZA (1) ZA974893B (en)

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AU4394799A (en) 1998-07-01 2000-01-24 Takeda Chemical Industries Ltd. Retinoid-associated receptor regulators
ES2216625T3 (en) 1998-11-27 2004-10-16 ABBOTT GMBH & CO. KG SUBSTITUTED BENCIMIDAZOLS AND THEIR EMPLOYMENT AS PARP INHIBITORS.
ES2151442B1 (en) * 1999-01-11 2001-07-01 Espanola Prod Quimicos NEW DERIVATIVE OF BENCENOETHANOL.
US6826561B2 (en) 2000-05-22 2004-11-30 Broadcom Corporation Method and apparatus for performing a binary search on an expanded tree
RU2288917C2 (en) * 2002-04-19 2006-12-10 Фаэс Фарма, С.А. POLYMORPH OF 4-[2-[4-[1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL]-PIPERIDINYL]ETHYL]-α,α-DIMETHYLBENZENEACETIC ACID, METHOD FOR ITS PREPARING, PHARMACEUTICAL PREPARATION BASED ON THEREOF AND ITS USING
CA2484460C (en) * 2002-04-19 2009-09-29 Faes Farma, S.A. Polymorph of 4-[2-[4-[1-(2-ethoxyethyl)-1h-benzimidazole-2-yl]-1-piperidinyl]ethyl]-.alpha..alpha. dimethyl-benzeneacetic acid
AU2003245442B2 (en) * 2002-06-13 2009-02-05 Vertex Pharmaceuticals Incorporated 2-ureido-6-heteroaryl-3h-benzoimidazole-4-carboxylic acid derivatives and related compounds as gyrase and/or topoisomerase IV inhibitors for the treatment of bacterial infections
US20070188330A1 (en) * 2006-01-24 2007-08-16 Morhard Robert C System and method for detecting, monitoring, tracking and identifying explosive materials using ID marks
US7247623B2 (en) * 2005-08-19 2007-07-24 Inspire Pharmaceuticals, Inc. Method of treating dry eye disease with non-drying antihistamines
CN104402773A (en) * 2008-02-12 2015-03-11 柳韩洋行 Preparation method and intermediate compound of 2-methyl-2'-phenylpropionic acid derivative
JP2010013472A (en) * 2009-09-09 2010-01-21 Faes Farma Sa POLYMORPH OF 4-[2-[1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL]-1-PIPERIDINYL] ETHYL-alpha,alpha-DIMETHYL BENZENOACETIC ACID
CN102675101B (en) * 2012-05-16 2014-01-29 王蕾 Preparation method of 2-(4-haloethyl) phenyl-2-methyl propionic ester and synthesis method of bilastine
CZ307500B6 (en) 2012-08-15 2018-10-24 Zentiva, K.S. A method of the preparation of a 2-methyl-2'-phenylpropionic acid derivative employing novel intermediates
RU2671577C2 (en) * 2013-03-15 2018-11-02 Геркулес Ллк Composition and method of producing personal care compositions with improved deposition properties
CN103214454A (en) * 2013-03-30 2013-07-24 北京万全德众医药生物技术有限公司 Bilastine crystal and preparation method thereof
CN103214455B (en) * 2013-03-30 2018-08-31 北京万全德众医药生物技术有限公司 A kind of preparation method of bilastine
WO2014188453A2 (en) * 2013-05-24 2014-11-27 Msn Laboratories Private Limited Novel process for the preparation of 2-[4-(2-{4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]-1-piperidinyl}ethyl) phenyl]-2-methylpropanoic acid
CN103351380B (en) * 2013-06-30 2019-01-22 北京万全德众医药生物技术有限公司 A method of preparing bilastine
CN104447683A (en) * 2013-09-12 2015-03-25 天津市汉康医药生物技术有限公司 Stable Bilastine compound
CN103896915A (en) * 2014-04-01 2014-07-02 中国药科大学 Benzimidazole derivative and preparation method thereof as well as application of benzimidazole derivative in medicine
EP3040334A1 (en) 2014-12-29 2016-07-06 Faes Farma, S.A. New benzimidazole derivatives as antihistamine agents
CN106349214B (en) * 2015-07-13 2020-11-03 南京长澳医药科技有限公司 Preparation method of bilastine impurity
LT3327012T (en) * 2015-07-24 2021-09-10 Urquima, S.A. CRYSTALLINE FORMS OF BILASTINE AND THEIR MANUFACTURING METHODS
CN105272977A (en) * 2015-09-19 2016-01-27 万全万特制药江苏有限公司 Bilastine intermediate preparation method
EP3170816A1 (en) 2015-11-20 2017-05-24 Faes Farma, S.A. Supersaturated compositions of benzimidazole compounds
EP3170817A1 (en) 2015-11-20 2017-05-24 Faes Farma, S.A. Co-crystals of benzimidazole compounds
WO2017167949A1 (en) 2016-04-01 2017-10-05 Krka, D.D., Novo Mesto Crystalline forms of bilastine
EP3452462A4 (en) * 2016-05-05 2019-10-23 MSN Laboratories Private Limited, R&D Center SOLID STATE FORMS OF 2- [4- (2- {4- [1- (2-ETHOXYETHYL) -1H-BENZIMIDAZOL-2-YL] -1-PIPERIDINYL} ETHYL) PHENYL] -2-METHYLPROPANOIC ACID AND PREPARATION METHOD THEREOF
CN107365298A (en) * 2017-03-14 2017-11-21 罗欣生物科技（上海）有限公司 A kind of preparation method of the benzyl propionate derivant of 2 methyl 2 '
CN109456316A (en) * 2017-09-06 2019-03-12 万全万特制药江苏有限公司 A kind of preparation method of bilastine impurity
ES2813561T3 (en) 2017-09-07 2021-03-24 Tiefenbacher Alfred E Gmbh & Co Kg Pharmaceutical composition in tablet comprising bilastine
CA3079303A1 (en) 2017-10-16 2019-04-25 Faes Farma, S.A. Aqueous compositions comprising bilastine and mometasone
WO2019097091A1 (en) 2017-12-18 2019-05-23 Alfred E. Tiefenbacher (Gmbh & Co. Kg) Pharmaceutical tablet composition comprising bilastine form 3 and a water-soluble filler
EP3470062B1 (en) 2017-12-18 2020-10-28 Alfred E. Tiefenbacher (GmbH & Co. KG) Pharmaceutical tablet composition comprising bilastine polymorphic form 3 and magnesium aluminometasilicate
US20210128544A1 (en) 2018-01-18 2021-05-06 Faes Farma, S.A. Ophthalmic compositions comprising bilastine, a beta-cyclodextrin and at least one gelling agent
CN109081827A (en) * 2018-11-06 2018-12-25 北京天弘天达医药科技股份有限公司 A kind of preparation method and application of bilastine
EP3725298A1 (en) 2019-04-16 2020-10-21 Faes Farma, S.A. Stable and preserved pharmaceutical compositions of bilastine
CR20230109A (en) 2020-07-30 2023-05-11 Faes Farma Sa Decongestant drug delivery system
CN112110893A (en) * 2020-10-28 2020-12-22 山东齐环医药科技有限公司 Preparation method of bilastine
EP4247331B1 (en) 2020-11-18 2025-10-08 BioPharma Synergies, S. L. Orodispersible powder composition comprising an antihistamine compound
EP4267109A1 (en) 2020-12-23 2023-11-01 Noucor Health S.A. A non-micronized bilastine composition
MX2024009978A (en) 2022-02-17 2024-08-26 Faes Farma Sa Bilastine composition for once-daily parenteral administration.
WO2024224326A1 (en) * 2023-04-27 2024-10-31 Leiutis Pharmaceuticals Llp Liquid parenteral formulations of bilastine
WO2024224308A1 (en) * 2023-04-27 2024-10-31 Leiutis Pharmaceuticals Llp Liquid parenteral formulations of bilastine free of cyclodextrins

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8904174D0 (en) * 1989-02-23 1989-04-05 British Bio Technology Compounds
AU7759591A (en) * 1990-04-13 1991-11-11 Smithkline Beecham Corporation Substituted benzimidazoles
ES2048109B1 (en) * 1992-07-20 1994-12-16 Espanola Prod Quimicos PROCEDURE FOR THE PREPARATION OF NEW PIPERIDIC DERIVATIVES OF BENCIMIDAZOLE.
DE701443T1 (en) * 1992-08-03 1997-01-30 Georgetown University, Washington, D.C. Terfanadine metabolites and their optically pure isomers for the treatment of allegic diseases
EP2261208A1 (en) * 1993-06-25 2010-12-15 Aventisub II Inc. Intermediates for the preparation of antihistaminic 4-diphenylmethyl/diphenylmethoxy piperidine derivatives

Also Published As

Publication number Publication date
CA2206754C (en) 2007-01-23
NO2011008I1 (en) 2011-06-06
PL320358A1 (en) 1997-12-08
ES2124167B1 (en) 1999-09-16
JP4218991B2 (en) 2009-02-04
CN1176964A (en) 1998-03-25
DE122011000006I1 (en) 2011-06-16
ZA974893B (en) 1997-12-30
LU91798I2 (en) 2011-05-23
HRP970307B1 (en) 2002-02-28
SI0818454T1 (en) 2004-08-31
HRP970307A2 (en) 1998-04-30
TR199700464A2 (en) 1997-12-21
CA2206754A1 (en) 1997-12-04
HU9700997D0 (en) 1997-07-28
AU725700B2 (en) 2000-10-19
NO972525D0 (en) 1997-06-03
ES2124167A1 (en) 1999-01-16
JPH1059961A (en) 1998-03-03
DE69728608T2 (en) 2005-04-21
AU2467297A (en) 1997-12-11
FR11C0023I1 (en) 2011-08-19
FR11C0023I2 (en) 2012-03-16
HU227598B1 (en) 2011-09-28
CZ289278B6 (en) 2001-12-12
NO2011008I2 (en) 2012-05-14
EP0818454A1 (en) 1998-01-14
CN1105716C (en) 2003-04-16
NO313195B1 (en) 2002-08-26
TR199700464A3 (en) 1997-12-21
CZ172397A3 (en) 1997-12-17
MXPA97004127A (en) 2005-07-25
BR9703276A (en) 2004-08-17
PT818454E (en) 2004-08-31
RU2182150C2 (en) 2002-05-10
DE69728608D1 (en) 2004-05-19
TW438794B (en) 2001-06-07
ATE264317T1 (en) 2004-04-15
DK0818454T3 (en) 2004-07-12
PL188908B1 (en) 2005-05-31
US5877187A (en) 1999-03-02
NO972525L (en) 1997-12-05
HUP9700997A1 (en) 1999-09-28
IN186319B (en) 2001-08-04
EP0818454B1 (en) 2004-04-14

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